KR950701317A - Indole Derivative - Google Patents

Abstract

The present invention provides indole derivatives of the general formula:

Indole derivatives of the present invention have potent antiestrogens activity and are useful as agents for the treatment of estrogen diseases such as ovulation infertility, prostate hyperplasia, osteoporosis, breast cancer, endometrial cancer and melanoma.

Description

Indole Derivative

Since this is an open matter, no full text was included.

Claims (8)

Indole derivatives of the general formula: [Wherein, R ¹ is a halogen atom, R ² is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a benzoyl group, R ³ is a hydrogen atom, a lower alkyl group or a halogen atom, and R ⁴ is a thienyl group or a general formula Wherein R ⁶ is a lower alkyl group, a cycloalkyl group, a phenyl group which may optionally have a lower alkyl group as a substituent, a phenyl-lower alkyl group or a pyridyl group, R ⁷ is a hydrogen atom or a lower alkyl group, Q is a sulfur or selenium atom and n is a group of an integer of 0 ~ 2), a is an alkylene group, m is an integer of 0 ~ 1, R ⁵ is, m is 0, as a hydrogen atom, an alkyl group, or a substituent hydroxyl group or general Formula -OBR ⁸ wherein B is a lower alkylene group and R ⁸ is phenyl, di-lower alkyl-amino, 1-pyrrolidinyl, piperidino, 1-imidazolyl or 1, 2, 4-triazole- R ⁵ is a lower alkoxycarbonyl group, carboxyl group, hydroxyl group, general formula -C (= O) -N (R ⁹ ) -R ¹⁰ (wherein R ⁹ and R ¹⁰ are the same or different and are each a hydrogen atom, a lower alkyl group, a cycloalkyl group with a benzene ring may be fused or fused, optionally, Group, a phenyl-or a lower alkyl group or a lower alkylsulfonyl group, R ⁹ and R ¹⁰ directly or in combination with each other via an oxygen or sulfur atom, together with the adjacent nitrogen atom, lower alkoxycarbonyl or heterocyclic ring which may be optionally substituted with a carboxyl group A group of formula -CH ₂ -N (R ¹¹ ) -R ¹² , wherein R ¹¹ and R ¹² are the same or different and may each optionally have a hydrogen atom, a lower alkyl group and a condensed benzene ring Or a cycloalkyl group, a phenyl group, a phenyl lower alkyl group or a lower alkanoyl group, or R ¹¹ and R ¹² may be directly substituted with each other directly or through an oxygen or sulfur atom and optionally substituted with a lower alkoxycarbonyl or carboxyl group with adjacent nitrogen atoms. Group of the heterocyclic group, general formula -OR ¹³ (wherein R ¹³ is a lower alkylcarbamoylphenyl group, a lower alkylaminomethylphenyl group, a lower alkylaminomethylphenyl group, Optionally a hydroxyl group, a lower group as a group or a substituent of 1-pyrrolidinylcarbonylphenyl group, 1-pyrrolidinylmethylphenyl group, 2-di-lower alkylaminoethyl group or 2-hydroxy-2-lower alkylaminoethyl group) Is a phenyl group which may have an alkoxy group, 1-pyrrolidinylcarbonyl or 1-pyrrolidinylmethyl group, and x is an integer of 0 to 2]. The compound of claim 1, wherein R ² is a hydrogen atom, R ³ is a hydrogen atom or a lower alkyl group, and R ⁴ is a general formula Wherein R ⁶ is a lower alkyl group, a cycloalkyl group, a group of a phenyl group, a phenyl-lower alkyl group or a pyridyl group which may optionally have one or more lower alkyl groups as substituents, and m is 1; 3. A compound according to claim 2, wherein R ⁵ is of the formula -C (= 0) -N (R ⁹ ) -R ¹⁰ wherein R ⁹ and R ¹⁰ are the same or different and each hydrogen atom, lower alkyl group, benzene ring is condensed May be a cycloalkyl group, a phenyl group, a phenyl-lower alkyl group or a lower alkylsulfonyl group, or R ⁹ and R ¹⁰ are bonded to each other directly or through an oxygen or sulfur atom, optionally with a lower alkoxycarbonyl or carboxyl group, with adjacent nitrogen atoms A group of a heterocyclic group which may be substituted, and the general formula —CH ₂ —N (R ¹¹ ) —R ¹² , wherein R ¹¹ and R ¹² are the same or different and each hydrogen atom, lower alkyl group, or benzene ring Is a cycloalkyl group, phenyl group, phenyl lower alkyl group or lower alkanoyl group which may be optionally condensed, or R ¹¹ and R ¹² are bonded to each other directly or through an oxygen or sulfur atom, together with a adjacent nitrogen atom, a lower alkoxycarbonyl or carboxyl group To be optionally substituted Heterocyclic group of indole derivatives to form a ring) that. The indole derivative of claim 1 wherein [Wherein R ³ is a hydrogen atom, a lower alkyl group or a halogen atom, R ⁶ is a lower alkyl group, a cycloalkyl group, a phenyl group which may optionally have one or more lower alkyl groups as substituents, a phenyl-lower alkyl group or a pyridyl group, R ¹¹ and R ¹² is the same or different and each is a cycloalkyl group, a phenyl group, a phenyl-lower alkyl group or a lower alkanoyl group in which a hydrogen atom, a lower alkyl group or a benzene ring may be optionally condensed, or R ¹¹ and R ¹² are directly or an oxygen or sulfur atom And combine with each other to form a heterocyclic group which may optionally be substituted with a lower alkoxycarbonyl or carboxyl group with adjacent nitrogen atoms. An estrogen inhibitor containing the indole derivative of claim 1 as an active ingredient. An estrogen inhibitor containing the indole derivative of claim 3 as an active ingredient. An estrogen inhibitor containing the indole derivative of claim 4 as an active ingredient. A method for treating estrogen disorders, comprising administering to a patient a pharmaceutically effective amount of the estrogen inhibitor of claim 5. ※ Note: The disclosure is based on the initial application.